Ethnopharmacological relevance: 22β-hydroxytingenone (22-HTG) is a quinonemethide triterpene isolated from Salacia impressifolia (Miers) A. C. Smith (family Celastraceae), which has been used in traditional medicine to treat a variety of diseases, including dengue, renal infections, rheumatism and cancer. However, the anticancer effects of 22-HTG and the underlying molecular mechanisms in melanoma cells have no...
Background: A new strain of human coronavirus (HCoV) spread rapidly around the world. Diabetes and obesity are associated with a worse prognosis in these patients. Congenital Generalized Lipodystrophy (CGL) patients generally have poorly controlled diabetes and require extremely high doses of insulin. There is no documentation in the literature of cases of COVID in CGL patients. Thus, we aimed to evaluate the p...
Cancer is still a major barrier to life expectancy increase worldwide, and hematologic neoplasms represent a relevant percentage of cancer incidence rates. Tumor dependence of continuous proliferative signals mediated through protein kinases overexpression instigated increased strategies of kinase inhibition in the oncologic practice over the last couple decades, and in this review, we focused our discussion on...
Gastric adenocarcinoma has high incidence and mortality rates worldwide. The aim of this study was to evaluate the antitumor activity of benzothiazole AFN01 against ACP03 gastric adenocarcinoma cell line. Furthermore, computational prediction of the pharmacokinetics and pharmacodynamics of this molecule and the molecular docking with the relevant pharmacological target found were performed. The MTT assay was pe...
Experimental oncology is based on a model of study through cell culture, a technique frequently used for the study of cancer biology and for tests of new anticancer therapies. This model provides an appropriate system for researching the effects of drugs and toxic compounds on cells, mutagenesis and carcinogenesis, in drug screening and development. In addition the cell lines allows consistent and reproducible ...
In the present study, in vitro techniques were used to investigate a range of biological activities of known natural quassinoids isobrucein B (1) and neosergeolide (2), known semi-synthetic derivative 1,12-diacetylisobrucein B (3), and a new semi-synthetic derivative, 12-acetylneosergeolide (4). These compounds were evaluated for general toxicity toward the brine shrimp species Artemia franciscana, cytotoxicity...
Federal University of Par?. Biological Science Institute. Laboratory of Experimental Neuropathology. Bel?m, PA, Brazil.; Federal University of Cear?. Drug Research and Development Center. Laboratory of Pharmacogenetics. Fortaleza, CE, Brazil.; Federal University of Par?. Biological Science Institute. Laboratory of Human Cytogenetics. Bel?m, PA, Brazil.; Federal University of Cear?. Drug Research and Development...
Lipid-based nanoparticle systems have been used as vehicles for chemotherapeutic agents in experimental cancer treatments. Those systems have generally been credited with attenuating the severe toxicity of chemotherapeutic agents. This study aimed to investigate the effects of associating paclitaxel (PTX) with a lipid-based nanoparticle system on a nonhuman primate, Cebus apella, documenting the toxicity as mea...
Federal University of Par?. Institute of Biological Sciences. Human Cytogenetics Laboratory. Bel?m, PA, Brazil.; Federal University of Par?. Institute of Biological Sciences. Human Cytogenetics Laboratory. Bel?m, PA, Brazil.; Federal University of Par?. Institute of Biological Sciences. Human Cytogenetics Laboratory. Bel?m, PA, Brazil.; University of S?o Paulo. Heart Institute. Medical School Hospital. S?o Paul...
With the aim of discovering new anticancer agents, we have designed and synthesized novel 6-hydroxy-benzo[d][1,3]oxathiol-2-one Schiff bases. The synthesis started with the selective nitration at 5-position of 6-hydroxybenzo[d][1,3]oxathiol-2-one (1) leading to the nitro derivative 2. The nitro group of 2 was reduced to give the amino intermediate 3. Schiff bases 4a–r were obtained from coupling reactions betwe...